O6-benzylguanine and BCNU in multiple myeloma: a phase II trial

Cancer Chemother Pharmacol. 2007 Aug;60(3):415-21. doi: 10.1007/s00280-007-0442-7. Epub 2007 Mar 13.

Abstract

Purpose: Carmustine (BCNU) is known to have modest activity in multiple myeloma; however, resistance to BCNU manifests by the activity of O6-methylguanine methyltransferase (MGMT). The objective of this study was to determine the safety and efficacy of depletion of MGMT activity in plasma cells using O6-benzylguanine (O6-BG) with BCNU in patients with multiple myeloma.

Methods: Patients with previously treated or untreated multiple myeloma were eligible. Cycles of O6-BG at a dose of 120 mg/m2 and BCNU at a dose of 40 mg/m2 were repeated every 6 weeks.

Results: Seventeen patients were enrolled on the study, with a median follow-up of 24.5 (range 5-69) months. One complete response (7%) and 3 partial responses (20%) were observed. Nine patients (60%) had stable disease. Bone marrow studies demonstrated 94% depletion of MGMT activity in CD38+ marrow cells. The most frequent grade 3 and 4 adverse events were neutropenia (71%), lymphocytopenia (53%), and thrombocytopenia (53%).

Conclusions: Chemotherapy utilizing the MGMT inhibitor O6-benzylguanine and BCNU results in inhibition of MGMT activity in malignant plasma cells and produces meaningful responses in a modest proportion of patients with multiple myeloma. Hematologic toxicity with this regimen is significant and dose-limiting.

Publication types

  • Clinical Trial, Phase III
  • Research Support, N.I.H., Extramural

MeSH terms

  • Adult
  • Aged
  • Antineoplastic Combined Chemotherapy Protocols / administration & dosage
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use*
  • Antineoplastic Combined Chemotherapy Protocols / toxicity
  • Carmustine / administration & dosage
  • Carmustine / therapeutic use
  • Carmustine / toxicity
  • DNA / blood
  • Drug Administration Schedule
  • Female
  • Follow-Up Studies
  • Guanine / administration & dosage
  • Guanine / analogs & derivatives
  • Guanine / therapeutic use
  • Guanine / toxicity
  • Humans
  • Male
  • Middle Aged
  • Multiple Myeloma / drug therapy*
  • Patient Selection
  • Reference Values

Substances

  • O(6)-benzylguanine
  • Guanine
  • DNA
  • Carmustine